General platform for systematic quantitative evaluation of small-molecule permeability in bacteria.

ABSTRACT: The chemical features that impact small-molecule permeability across bacterial membranes are poorly understood, and the resulting lack of tools to predict permeability presents a major obstacle to the discovery and development of novel antibiotics. Antibacterials are known to have vastly different structural and physicochemical properties compared to nonantiinfective drugs, as illustrated herein by principal component analysis (PCA). To understand how these properties influence bacterial permeability, we have developed a systematic approach to evaluate the penetration of diverse compounds into bacteria with distinct cellular envelopes. Intracellular compound accumulation is quantitated using LC-MS/MS, then PCA and Pearson pairwise correlations are used to identify structural and physicoche

SUBMITTER: Davis TD 

PROVIDER: S-EPMC4245172 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature